Parasiticidal lotions



Patented Dec. 29, 1953 UNITED srArss PARASITICIDAL LOTIONS No Drawing. Application September 18, 1947, Serial No. 774,894

2 Claims.

The present invention relates to parasiticidal lotions for combating such body parasites as head and body lice.

Among the objects of the present invention is to provide a lotion which is quickly effective as a parasiticide, which is clear, homogeneous and stable, which manifests no adverse skin reaction, which is easy to apply and easy to remove, which is free from grease and which in general lends itself satisfactorily to the strictest pharmaceutical requirements.

In accordance with certa n features of the present invention, the lotion comprises an aqueous suspension made of a pyrethrum extract as an active parasiticidal ingredient, a sesamin extract having a synergistic or activating action on the pyrethrins of the pyrethrum extract, apiol having insecticidal effect, dinitroanisole serving as an ovicide and benzyl alcohol which is a solvent for the ovicide and which affords an anaesthetic effect. The mixture also preferably contains perfume oils.

This mixture may be clear or cloudy depending for the most part on the wax content of the pyrethrum extract and on the solvent used in the manufacture of this extract. The dewaxed purified pyrethrum extract as used for aerosol bombs yields mostly clear mixtures.

In order to make the mixture described above emulsifiable, an intermiscible solvent has to be used. The solvent may be either oleic acid or a glycol fatty acid ester such as propylene glycol monolaurate or propylene glycol monooleate.

The resulting solution must be emulsified in water. The emulsifying agents for that purpose must be slightly acid and acid-stable to produce a lotion having a final pH of approximately 5.5-6.5 which is the range of optimum stability of pyrethrins. The emulsifying agents are desirably a combination of the following:

1. Sulfonated or sulfated oils such as castor oil, corn oil, cottonseed oil, etc.

2. Derivatives of hexahydric alcohol anhydride partial esters, namely sorbitan or mannitan monolaurate, such compounds being condensation products with ethylene oxide. The sum of such ethylene oxide linkages add up to 20 mole per mol of sorbitan or mannitan monolaurate.

3. Dioctyl sulfosuccinate and desirably the sodium salt, such as that described in the U. S. r

Patent #2,028,091.

For example, sulfonated oil may be combined with dioctyl sodium sulfosuccinate; sulfonated oil with derivatives of hexahydric alcohol anhydride partial esters; or the latter compound with 2 dioctyl sodium sulfosuccinate to produce the necessary emulsification.

The different ingredients of the lotion are dispersed in a diluent such as water. The resulting mixture aside from the emulsifying agents and the intermiscible solvent is not clear or stable, since it comprises a number of immiscible liquids. Therefore, to bring all of the ingredients of the mixture with water together in the form of a clear and stable emulsion, it has been found advantageous to employ two emulsifying agents and an intermiscible solvent.

The pyrethrum extract containing pyrethrins may be of any suitable type, and is desirably a dewaxed product containing about 20% pyrethrins. If the pyrethrum extract used yields a cloudy lotion, this can be corrected to produce a clear product by the use of additional organic solvents in a concentration of not more than 2% by weight at the expense of the water content of the formula. These solvents should be of such a nature as to prevent the waxes and polymerization products, as found in the commercially available pyrethrum extract, from precipitating out of the lotion. These solvents may be, for example, acetone, cyclohexanone, carbon tetrachloride, chloroform, alkylated naphthalenes and others.

The sesamin extract may contain in total from 11 to 25% of sesamin solids. The sesamin solids desirably contain an average of of pure sesamin.

The apiol (dimethyl methylene ether of allyl tetroxybenzene) which is employed is desirably oleoresin of parsley fruit (liquid apiol). Apiol in this form has the advantage of not crystallizing out of the lotion. However, as far as certain aspects of the invention are concerned, crystalline apiol may be employed, although for lotion purposes, it is not as desirable as liquid apiol.

The apiol can be dissolved in the pyrethrum extract since the latter contains kerosene as a dissolving medium, in which apiol is. also soluble.

Dinitroanisole is employed as an ovicide to destroy the nits or eggs of the parasites. Benzyl alcohol is used as a solvent for the dinitroanisole. This alcohol also has a slight anesthetic effect which is desirable. Benzyl alcohol is also desir able for use as a solvent for the dinitroanisole, because a suspension of pure sesamin crystals in sesame oil was found soluble in benzyl alcohol.

The odor of the lotion may be improved by using a mixture of essential oils.

The following examples are illustrations of formulations in accordance with the present invention, but they are not to be construed as I limiting the invention:

EXAMPLE 1 Using selfonated oil and dioctyl sodium sulfosuccinaie as emulsifying agents Percent weight/weight Pyrethrurn extr ct, dewaxed (20%. py-

rethrins) 5.0 Apiol (oleoresin parsley) 0.5 Sesainin extract 0.25 Propylene glycol monolaurate 8.0 Dioctyl-sodiurnsuliosuccinate 3.0- Sulionated corn oil, sulfonated castor oil or sulionated cottonseed oil 20,..0 ZA-dinitroanisole .m 1.0- Benzyl alcohol (free from chlorine) 3;.0. Perfume oils 1.0 Distilled water q .s. 100% (apron 53;.0).

EXAMPLE 2 Using sulfonated oil and derivatives of herahydric alcohol cmhydride partial esters Percent weight/weight Same as Example exceptthat propylene glycol monolaurate is replaced by ra. oleic. acid and; thewater adjusted accordingly;

EXAlvIEIiEe, Usingclerivotiuesofiiiercdhydric alcohol anhydridc partial, esters and dioctul. sodium? sulficsuccinate Per cent weight/weight Pyrethrum extract 5.0 Apiol 0.5 Sesamin extract 0.25 Propylene glycol monolaurate 6.0 ioctyl-sodium-suliosuccinate q. 18.0 Sorbitan or mannitan incnolaurate polyoxyalkylene derivatives 10.0, 2,-d-dinitroanisole. 1.0 Benzyl alcohol 8.0 Perfume oils 1.0. Distilled water. q, s. 100% (appn. 50.0) EXAMPLE 5 Same as Example dexcept that the propylene glycol monolaurate is replaced by cleic acid 3.5 and the water, is adjusted accordingly.

A procedure which may be employed for malring a batch of the. lotionin accordance withv the formulation above set. forth, is. as follows:

L Mix together dinitroanisole, sesamin. extract.

3. Add the two emulsifying agents and mix.

4. Add water and mix until a clear solution is obtained.

A pyrethrum lotion as described is thoroughly efiicient and quickly eilective in combating body and head lice, even in the most severe cases, is stabilized against decomposition, and remains clear and homogeneous indefinitely at temperatures above 15 C. When this lotion is applied,

. the. lice die. quickly. These applications are attended without dermatitis or skin irritation. The parasiticidal action of the lotion is decisive, and

its contactedwith this lotion are killed and fail to incubate.

In the application of the lotion, one or two ounces 0t this lotion, applied, as for example, to the infected head of a person, is allowed to remain for about ten to fifteen minutes. At the end of that period, the medication may be removed with water, or if desired, soap and water may be used. It was found by this medication sees, that the lice were killed, and that the nits did not incub at the end of the hatching period.

Since the lotion oi the invention is clear and homogeneous, it is not necessary to shale it before use. In the case oi a suspen on which has to be shaken before use, ther is no assurance that the active ingredients will applied to the aiie-cted part in the right proportions. Furthermore, with a suspension, there are solid partic which are not easy to wash on". The lotion 0. present invention, on the other hand, contains oetergents which serve to produce foam so that the lotion works like a shampoo. A great deal of foam is produced in its application, and this carries all foreign matter out of the hair. in other Words, the emulsifying agents serve not only to afford a clear lotion, but also permit said lotion with all the foreign matter-attached thereto to be l wa hed oil. This is important where hair is being treated.

While the invention has been described with particular reference to a specific embodiment, it is to be understood that it is not to be limited thereto but is to be construed broadly and restricted solely by the scope of the appended claims.

What is claimed is:

1'. A parasiticidal lotion for body parasites containing pyrethrurn extract, sesaniin extract, apiol, dinitroanisole, benzyl' alcohol, interiniscible solvent for said ingredients, water emulsifying agents to form a clear, stable, homogeneous lotion, said intermiscible solvent being oleic acid and said emulsifying agents including a sulfonated oil and dioctyl sulfosucoinate,

2. A parasiticidal lotion for body parasites containing pyrethrum extract, sesamin extract, apiol, dihitroanisole, benzyl alcohol, and intermiscible solvent for said ingredients, water and emulsifying agents to form a clear, stable, homogeneous lotion, said. intermiscible solvent being oleic acid and said. emulsifying agents including a derivative 01 hexa hydric, alcohol anhydride. partial esters and dioctyl suliosuccinate.

ALLEN L. OMOHUNDRO. FRANZ M. NEUMEIER.

References Cited in the file of this patent UNITED STATES PATENTS Number (Other references on following page) 5 UNITED STATES PATENTS Number Number Name Date Grant Dec. 19, 1933 Eagleson May 28', 1940 Hyman Apr. 25;, 1944 Park Oct. 29, 1946 Brown Dec. 6, 1947 FOREIGN PATENTS Country Date Great Britain 0015.2, 1945 France July 19, 1929 OTHER REFERENCES Goodman, Cosmetic Dermatology, page 10, Mc- Graw Hill Book Company. 1936, New York.

6 Hager, Handbuch der Pharmazeutischen Praxis, volume II, page 400, 1927, J. Springer Company.

Eddy, NRC Insect Control Committee Report No. 143, November 21, 1945; Committee on Medi- 5 cal Research OS'RD, Section 1 (OEM cmr 4331),

pages 1, 9, 10, 15 and 16.

Drug and Cosmetic Industry, January 1943, page 93.

J. A. P. A., Prao. Pharm. Ed., March 1945, pages 10 73 to 76.

Drug and Cosmetic Industry, May 1945, page 636.

Urologic and Cutaneous Review, May 1946, page 310. 15 

4. A PARASITICIDAL LOTION FOR BODY PARASITES CONTAINING PYRETHRUM EXTRACT, SESAMIN EXTRACT, APIOL, DINITROANISOLE, BENZYL ALCOHOL, AN INTERMISCIBLE SOLVENT FOR SAID INGREDIENTS, WATER AND EMULSIFYING AGENTS TO FORM A CLEAR, STABLE, HOMOGENEOUS LOTION, SAID INTERMISCIBLE SOLVENT BEING OLEIC ACID AND SAID EMULSIFYING AGENST INCLUDING A SULFONATED OIL AND DIOCTYL SULFOSUCCINATE. 